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Academia and Industry Members Helping to Advance Structure-Function Database of G-protein Coupled Receptors for Drug Discovery

Los Angeles and Shanghai, September 9, 2015 — The GPCR Consortium today announced the addition of four members from the pharmaceutical industry: Pfizer, Inc., H. Lundbeck A/S, Boehringer Ingelheim, and Taisho Pharmaceutical Co., Ltd. The GPCR Consortium originally planned for eight members; however, the demand exceeded expectations with nine members joining within the first year.

The GPCR Consortium is an international, nonprofit, open-source collaboration that comprises leading academic research institutes in the United States and China and major pharmaceutical companies from around the world. The GPCR Consortium was initiated in 2014 with the purpose of helping coordinate and manage the generation of high-resolution structure-function studies of medically important proteins known as G-protein coupled receptors (GPCRs) while making all data publically available.

More than 800 distinct GPCRs are found in the human body, where they carry out important cellular functions, including communication between cells and their environment. Malfunctions of GPCRs have been linked to conditions including multiple cancers, diabetes and mental health disorders. The data being generated by the GPCR Consortium are critical in understanding these processes at the molecular level and in helping to develop the next generation of GPCR-targeted drugs.

“Although GPCRs account for nearly 40 percent of the targets for current drugs, very little is known about their structure or mode of action,” said Dr. Tony Wood, Senior Vice President, Worldwide Medicinal Chemistry, Pfizer.“This pioneering, nonprofit initiative has brought together pharmaceutical companies and leading research institutes worldwide to advance a critical area of research necessary to improve drug discovery.”

“The GPCR Consortium will contribute valuable information to drug discovery efforts for pharma around the globe,” said Dr. Michel Pairet, Senior Corporate Vice President of Research and Nonclinical Development at Boehringer Ingelheim. “A more complete understanding of GPCR structure and function will facilitate the effective design and selection of new drug candidates.”

“We have now attained a critical mass that we feel is optimum to achieve our scientific goal of understanding at least 200 of the potentially most druggable GPCRs,” said Dr. Michael Hanson, president and cofounder of the GPCR Consortium. Dr. Hanson is widely recognized for his contributions to X-ray crystallography of GPCRs and other complex molecules.

“The higher than expected level of interest highlights the demand and importance of the data,” said Professor Raymond Stevens, cofounder of the GPCR Consortium and Professor at the iHuman Institute at ShanghaiTech University and Bridge Institute at the University of Southern California. “To date the companies involved have been great at sharing compounds and knowledge aiding in our precompetitive and basic science studies of GPCRs. It is wonderful to work in such a collaborative open-source industry-academia manner.”

“It is unusual to have such a diverse and global group of pharmaceutical companies working together,” said Klaus Bæk Simonsen, VP at Lundbeck, “but the precompetitive character of the GPCR Consortium makes it attractive and beneficial to both academic and industry members.”

“We are really pleased to have the unprecedented opportunity to advance the deep understanding of GPCR structure, although one of the major hurdles to obtaining structural information for GPCRs has been the difficulty in forming stable crystals,” said Dr. Shigeru Okuyama, Senior Executive Officer, Research and Development of Pharmaceutical Product at Taisho Pharmaceutical Co., Ltd.

The consortium is actively seeking collaborations with other groups to help interpret and leverage the data to further understanding of GPCR ligand recognition and the many different intracellular molecules that interact with these processes.

Amgen, Sanofi and ONO are the founding members of the GPCR Consortium; Novo Nordisk and Merck & Co., Inc. joined in February 2015. The research is currently at the following three leading academic sites: iHuman Institute at ShanghaiTech University, Shanghai Institute of Materia Medica, a member of the Chinese Academy of Sciences, and the Bridge Institute at theUniversity of Southern California in Los Angeles.